Lead generation is increasingly seen as a distinct and
success-determining phase of the drug discovery process. Over
recent years, there have been major advances in the understanding
of what constitutes a good lead compound and how to improve the
chances of finding such a compound. Written by leading scientists
and established opinion leaders from industry and academia, this
book provides an authoritative overview of the field, as well as
the theory, practice, and scope, of the principal Lead
Generation Approaches in Drug Discovery, including:

The evolution of the lead discovery process, key concepts,
current challenges, and future directions

Strategies and technologies driving the high-throughput
screening (HTS) approach to lead discovery, including the shifting
paradigms in the design of compound collections and best practice
in the hit confirmation process

Knowledge-based in silico or "virtual" screening

Theory and practice of the fragment-based approach to lead
discovery

The opportunities and challenges presented by multi-target drug
discovery (MTDD)

De novo design of lead compounds and new approaches to
estimating the synthetic accessibility of de novo–designed
molecules

The impact of natural products on drug discovery, and potential
of natural product–like compounds for exploring regions of
biologically relevant chemical space

Using early screening of hits and leads for metabolic,
pharmacokinetic, and toxicological liabilities to reduce attrition
during the later phases of drug discovery

The utility of parallel synthesis and purification in lead
discovery

With each topic supported by numerous case studies, this is
indispensable reading for researchers in industry and academia who
wish to keep up to date with the latest strategies and approaches
in drug discovery.

ZORAN RANKOVIC is a Senior Research Fellow and
Associate Director in Medicinal Chemistry at Schering-Plough
Research Institute, UK. He received his PhD in organic chemistry
from the University of Leeds (UK) before starting his medicinal
chemistry career in 1995 at Organon, UK. Since then, working on
projects over a range of therapeutic areas, including psychosis,
analgesia, and cardiovascular and bone diseases, he gained
extensive experience in all stages of the drug discovery process,
including lead generation. From this work, Dr. Rankovic has
authored or coauthored over fifty scientific publications, book
chapters, and patents, and has given invited lectures at numerous
international conferences.

RICHARD MORPHY is a medicinal chemistry section head at
Schering-Plough Research Institute (SPRI) at Newhouse, Scotland. He
has twenty years' experience in the pharmaceutical industry,
previously working for Celltech and Organon on a wide range of
oncology, inflammation, psychiatry, and analgesia projects. In
addition to his extensive experience of the lead discovery process,
he has a keen interest in the development of medicinal chemistry in
emerging economies and is an opinion leader in the area of
multi-target drug discovery.

"The book provides a comprehensive overview of many aspects of the
lead generation process . . . The book delivers a good introduction
to the process of lead generation for novice researchers. It is
also useful for more experienced scientists to update their
knowledge and/or to identify some new details." (ChemMedChem,
October 2010)

"This volume is recommended to chemists and biologists who wish
to learn about the practice of high throughput screening and about
the concepts involved in making the method a successful route to
drug discovery." (Journal of Medicinal Chemistry, 2010)"Each
chapter provides a comprehensive overview of one aspect of the lead
generation process. To get more indepth knowledge, extensive
references including recent publications are given."
(ChemMedChem, 2010)

Digital version available through Wiley Online Library

Instructors

Permissions

To apply for permission please send your request to permissions@wiley.com with
specific details of your requirements. This should include, the Wiley title(s), and the specific portion of the content you wish to re-use
(e.g figure, table, text extract, chapter, page numbers etc), the way in which you wish to re-use it, the circulation/print run/number of people
who will have access to the content and whether this is for commercial or academic purposes. If this is a republication request please include details
of the new work in which the Wiley content will appear.